Filorexant - CAS 1088991-73-4
Catalog number: 1088991-73-4
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Orexin Receptor (OX Receptor)
Filorexant, a selective reversible and orally bioavaliable antagonist of OX(1)R receptor and OX(2)R receptor, could probably be an effective compound in the treatment of insomnia. It is still under the Phase II trial by Merck. Binding Ki: less than 3 nM.
10 mM in DMSO
-20ºC Freeze
Filorexant, a selective reversible and orally bioavaliable antagonist of OX(1)R receptor and OX(2)R receptor, could probably be an effective compound in the treatment of insomnia.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Canonical SMILES:
Current Developer:
Merck & Co
1.Current Phase II investigational therapies for insomnia.
Zisapel N Expert Opin Investig Drugs. 2015 Mar;24(3):401-11. doi: 10.1517/13543784.2015.987340. Epub 2014 Nov 25.
INTRODUCTION: ;Insomnia is typified by a difficulty in sleep initiation, maintenance and/or quality (non-restorative sleep) resulting in significant daytime distress.;AREAS COVERED: ;This review summarizes the available efficacy and safety data for drugs currently in the pipeline for treating insomnia. Specifically, the authors performed MEDLINE and internet searches using the keywords 'Phase II' and 'insomnia'. The drugs covered target GABAA (zaleplon-CR, lorediplon, EVT-201), orexin (filorexant, MIN-202), histamine-H1 (LY2624803), serotonin 5-HT2A (ITI-007), melatonin/serotonin5-HT1A (piromelatine) and melatonin (indication expansions of prolonged-release melatonin and tasimelteon for pediatric sleep and circadian rhythm disorders) receptors.;EXPERT OPINION: ;Low-priced generic environments and high development costs limit the further development of drugs that treat insomnia. However, the bidirectional link between sleep and certain comorbidities may encourage development of specific drugs for comorbid insomnia. New insomnia therapies will most likely move away from GABAAR receptors' modulation to more subtle neurological pathways that regulate the sleep-wake cycle.
2.Orexin in sleep, addiction and more: is the perfect insomnia drug at hand?
Hoyer D;Jacobson LH Neuropeptides. 2013 Dec;47(6):477-88. doi: 10.1016/j.npep.2013.10.009. Epub 2013 Oct 23.
Orexins A and B (hypocretins 1 and 2) and their two receptors (OX1R and OX2R) were discovered in 1998 by two different groups. Orexin A and B are derived from the differential processing of a common precursor, the prepro-orexin peptide. The neuropeptides are expressed in a few thousand cells located in the lateral hypothalamus (LH), but their projections and receptor distribution are widespread throughout the brain. Remarkably, prepro peptide and double (OX1R/OX2R) receptor knock out (KO) mice reproduce a sleep phenotype known in humans and dogs as narcolepsy/cataplexy. In humans, this disease is characterized by the absence of orexin producing cells in the LH, and severely depleted levels of orexin the cerebrospinal fluid. Null mutation of the individual OX1R or OX2R in mice substantially ameliorates the narcolepsy/cataplexy phenotype compared to the OX1R/OX2R KO, and highlights specific roles of the individual receptors in sleep architecture, the OX1R KO demonstrating an a attenuated sleep phenotype relative to the OX2R KO. It has therefore been suggested that orexin is a master regulator of the sleep-wake cycle, with high activity of the LH orexin cells during wake and almost none during sleep.
3.Optical Probing of Orexin/Hypocretin Receptor Antagonists.
Li SB;Nevárez N;Giardino WJ;de Lecea L Sleep. 2018 Jul 27. doi: 10.1093/sleep/zsy141. [Epub ahead of print]
Study Objectives: ;The present study investigated the function of Hypocretin (Hcrt or Orexin/OX) receptor antagonists in sleep modulation and memory function with optical methods in transgenic mice.;Methods: ;We used Hcrt-IRES-Cre knock-in mice and AAV vectors expressing channelrhodopsin-2 (ChR2) to render Hcrt neurons sensitive to blue light stimulation. We optogenetically stimulated Hcrt neurons and measured latencies to wakefulness in the presence or absence of OX1/2R antagonists and Zolpidem. We also examined endogenous Hcrt neuronal activity with fiber photometry. Changes in memory after optogenetic sleep disruption were evaluated by the novel object recognition test (NOR) and compared for groups treated with vehicle, OX1/2R antagonists, or Zolpidem. We also analyzed EEG power spectra of wakefulness, rapid eye movement (REM) sleep, and non-REM (NREM) sleep following the injections of vehicle, OX1/2R antagonists, and Zolpidem in young adult mice.;Results: ;Acute optogenetic stimulation of Hcrt neurons at different frequencies resulted in wakefulness. Treatment with dual OX1/2R antagonists (DORAs) DORA12 and MK6096, as well as selective OX2R antagonist MK1064 and Zolpidem, but not selective OX1R antagonist 1SORA1, significantly reduced the bout length of optogenetic stimulation-evoked wakefulness episode.
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